Vasodilatación inducida por Croton schiedeanus Schlecht vinculada con la ruta metabólica de guanilato ciclasa

  1. Chaves Torres, Marlén 1
  2. Puebla Ibáñez, Pilar 2
  3. Guerrero Pabón, Mario 3
  1. 1 Universidad Militar Nueva Granada Pontificia Universidad Javeriana
  2. 2 Universidad de Salamanca
    info

    Universidad de Salamanca

    Salamanca, España

    ROR https://ror.org/02f40zc51

  3. 3 Universidad Nacional de Colombia
    info

    Universidad Nacional de Colombia

    Bogotá, Colombia

    ROR https://ror.org/059yx9a68

Show affiliations +
Journal:
Revista Colombiana de Ciencias Químico-Farmacéuticas

ISSN: 1909-6356,  0034-7418

Year of publication: 2012

Volume: 41

Issue: 1

Pages: 36-49

Type: Article

DIALNET GOOGLE SCHOLAR lock_openOpen access editor

More publications in: Revista Colombiana de Ciencias Químico-Farmacéuticas

Abstract

The EtOH extract of Croton shiedeanus Schlecht, medicinal species used by the popular tradition in Colombia for hypertension, relaxes vascular rings of Wistar rat aorta stimulated with phenylephrine (10-6 M, alpha adrenergic receptor agonist), in a dose-depending manner, with an EC50 of 1.3 × 10-5 g/mL. This effect is superior to that exercised over rings stimulated with KCl (6,0 × 10-2 M, voltage-dependent calcium channel activator) and is reduced in vascular rings without endothelium. The vascular relaxation is reversed in the presence of methylene blue (1.0 × 10-4 M, guanylate cyclase inhibitor) and L-NAME (10-4 M, nitric oxide synthase inhibitor), and is not affected in presence of propranolol (10-6 M, beta receptor antagonist), atropine (30 × 10-5 M, muscarinic antagonist) and indomethacin (10-6 M, cyclooxygenase inhibitor). Additionally, the contractions induced by CaCl2 (10-5 – 10-2 M, calcium currents activator) are not affected in the presence of EtOH C. schiedeanus extract (5.0 × 10-5 g/mL). Serial dilutions of L-NAME and methylene blue (until 10-14 M) show that C. schiedeanus recovers almost entirely the vasodilator effect in presence of L-NAME but not in presence of methylene blue (91 versus 68% of Emax, respectively). In addition, the relaxant potency and efficacy of C. schiedeanus is greater than its predominant active metabolite, ayanin (IC50: 1,3 vs. 4,9 × 10-5 g/mL, Emax: 100 vs. 67%). These findings suggest that C. schiedeanus exerts vasodilating effects, particularly related to the metabolic pathway of guanylate cyclase and gives support the traditional use of this species.

Bibliographic References

  • A.M. Osorio, A. Rosenkrans, “Guía para el uso de animales de laboratorio”, 11. Departamento de Farmacia, Facultad de Ciencias, Universidad Nacional de Colombia, 1990.
  • A.V. Chobanian, G.L. Bakris, H.R. Black, W.C. Cushman, L.A. Green, J.L. Izzo, 8. D.W. Jones, B.J. Materson, S. Oparil, J.T. Wright, E.J. Roccella, Seventh report of the Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure, Hypertension, 42, 1206 (2003).
  • B. Mayer, F. Brunner, K. Schmidt, Inhibition of nitric oxide synthesis by methyl-12. ene blue, Biochem. Pharmacol., 45, 367 (1993).
  • B.T. Mellion, L.J. Ignarro, E.H. Ohlstein, E.G. Pontecorvo, A.L. Hyman, P.J. 15. Kadowitz, Evidence for the inhibitory role of guanosine 3’,5’-monophosphate in adp-induced human platelet aggregation, Blood, 57, 946 (1981).
  • D. Rees, R.M.J. Palmer, R. Schuls, Characterization of three inhibitors of 13. endothelial nitric oxide synthase in vitro and in vivo, Br. J. Pharmacol., 101, 746 (1990).
  • G. Loirand, P. Pacaud, C. Mironneau, J. Mironneau, Evidence for two distinct 18. calcium channels in rat vascular smooth muscle cells in short-term primary culture, Pflügers. Arch., 407, 566 (1986).
  • G. Yetik-Anacak, J.D. Catravas, Nitric oxide and the endothelium: History and 16. impact on cardiovascular disease, Vasc. Pharmacol., 45, 268 (2006).
  • H. García, “Flora medicinal de Colombia”, Instituto de Ciencias Naturales, 1. Bogotá, 1975, vol. 2, p. 87.
  • M.A. Marletta, Nitric oxide synthase structure and mechanism, 19. J. Biol. Chem., 268, 12231 (1993).
  • M.F. Guerrero, Elementos para la evaluación eficaz de productos naturales con 9. posibles efectos antihipertensivos, Biomédica, 29, 547 (2009).
  • M.F. Guerrero, P. Puebla, M.L. Martín, R. Carrón, L.S. Román, M.T. Reguero, 5. Inhibitory effect of N(G)-nitro-L-arginine methyl ester on the anti-adrenergic response elicited by ayanin in the pithed rat, Planta Med., 68, 322 (2002).
  • M.F. Guerrero, P. Puebla, R. Carrón, M.L. Martín, L. Arteaga, L.S. Román, 3. Assessment of the antihypertensive and vasodilator effects of ethanolic extracts of some Colombian medicinal plants, J. Ethnopharmacol., 80, 37 (2002).
  • M.F. Guerrero, P. Puebla, R. Carrón, M.L. Martín, L.S. Román, Quercetin 7. 3,7-dimethyl ether a vasorelaxant flavonoid isolated from Croton schiedeanus Schlecht, J. Pharm. Pharmacol., 54, 1373 (2002).
  • M.F. Guerrero, R. Carrón, M.L. Martín, L.S. Román, M.T. Reguero, Antihy-2. pertensive and vasorelaxant effects of aqueous extract from Croton schiedeanus Schlecht in rats, J. Ethnopharmacol., 75, 33 (2001).
  • R. Carrón, E. Sanz, P. Puebla, M.L. Martín, L.S. Román, M.F. Guerrero, Mech-6. anisms of relaxation induced by flavonoid ayanin in isolated aorta rings from Wistar rat, Colombia Med., 41, 10 (2010).
  • R. Tallarida, L. Jacob, “The dose-response relation in pharmacology”, Springer-10. Verlag Ed., New York, 1979, p. 111.
  • S. Moncada, E.A. Higgs, Endogenous nitric oxide physiology, pathology and 14. clinical relevance. Eur. J. Clin. Invest., 21, 361 (1991).
  • S.X. Correa, “Estudio fitoquímico y evaluación de la acción relajante vascular 4. de Croton schiedeanus Schlecht”, trabajo de grado, Departamento de Farmacia, Facultad de Ciencias, Universidad Nacional de Colombia, sede Bogotá (2004).
  • V. Bayard, F. Chamorro, J. Motta, N.K. Hollenberg, Does flavanol intake influ-17. ence mortality from nitric oxide-dependent processes? Ischemic heart disease, stroke, diabetes mellitus, and cancer in Panamá, Int. J. Med. Sci., 4, 53 (2007).
Data source: Dialnet